SUBSTITUTED 3-ARYLSULFONYL-PYRAZOLO[1,5-a]PYRIMIDINES, SEROTONIN 5-HT RECEPTOR ANTAGONISTS, METHODS OF PRODUCING AND USING SAID COMPOUNDS Russian patent published in 2010 - IPC C07D487/04 A61K31/519 A61P25/28 A61P25/18 A61P25/24 A61P3/06 

Abstract RU 2393158 C1

FIELD: chemistry.

SUBSTANCE: present invention relates to novel substituted 3-arylsulfonyl-pyrazolo[1,5-a]pyrimidines of general formula 1, their pharmaceutically acceptable salts and/or hydrates having serotonin 5-HT6 receptor antagonist properties. The compounds can be used in treating and preventing various diseases of the central nervous system, pathogenesis of which is associated with 5-HT6 receptors, particularly cognitive disorders, neurodegenerative diseases and psychiatric disorders. The compounds have anxiolytic and nootropic effect and can also be used for preventing and treating anxiety disorder and for enhancing metal capacity. In formula 1 , R1 is a hydrogen atom, C1-C3 alkyl, (C1-C3)alkyloxy(C1-C3)alkyl, hydroxy(C1-C3)alkyl, pyridyl; R2 is a hydrogen atom, halogen atom, C1-C3 alkyl, phenyloxy or pyridyloxy; R3 is a hydrogen atom, C1-C3 alkyl, C1-C3 alkyloxy, (C1-C3)alkyloxy(C1-C3)alkyl, hydroxy(C1-C3)alkyl, pyridyl; R4 is C1-C3 alkyl; R5 is a hydrogen atom, one or two halogen atoms, C1-C3 alkyl, C1-C3 alkyloxy or hydroxyl; X is a sulphur atom or thionyl group (SO).

EFFECT: obtaining compounds which can be used in treating and preventing various diseases of the central nervous system.

24 cl, 9 dwg, 4 tbl, 19 ex

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RU 2 393 158 C1

Authors

Ivashchenko Aleksandr Vasil'Evich

Savchuk Nikolaj Filippovich

Ivashchenko Andrej Aleksandrovich

Dates

2010-06-27Published

2008-10-06Filed